作为医药中间体,用于相关药物合成(具体应用场景参考参考文献)。
医药
合成路线 1(1. 合成:85803-62-9)
产率:100%
合成条件:With potassium carbonate In water for 18 h; Heating / reflux
实验步骤:准备57; 2-(4-甲基哌嗪-1-戊二醛)2-氟苯甲醛(20.0mL,189.9mmol),1-甲基哌嗪(33.0mL,297.7mmol)和碳酸钾(40.0g,289.4mmol)的水(200mL)回流 冷却后,用EtOAc(2×150mL)萃取混合物。用盐水洗涤这些萃取物,用MgSO 4干燥并浓缩,得到PP57(38.6g,100%),为橙色油状物,其具有:NMR(CDCl 3) δ10.10(s,1H),7.77(dd,J = 7.9,1.7Hz,1H),7.51-7.48(符号,1H),7.10-7.06(m,2H),3.11(t, J = 4.6Hz,4H),2.63(br s,4H),2.36(s,3H)。
参考文献:
- [1] Patent: WO2006/48727, 2006, A1. Location in patent: Page/Page column 83 [2] Patent: US2003/87914, 2003, A1 [3] Russian Chemical Bulletin, 2004, vol. 53, # 6, p. 1240 - 1247 [4] Chemical Communications, 2017, vol. 53, # 75, p. 10448 - 10451 [5] Synthesis, 1987, # 7, p. 641 - 645 [6] Medicinal Chemistry Research, 2015, vol. 24, # 9, p. 3516 - 3528 [7] Journal of medicinal chemistry, 1983, vol. 26, # 8, p. 1116 - 1122 [8] Bioorganic and Medicinal Chemistry, 2006, vol. 14, # 8, p. 2498 - 2506 [9] Patent: US2004/254196, 2004, A1. Location in patent: Page 9 [10] Patent: WO2005/90300, 2005, A1. Location in patent: Page/Page column 30